Beta-lactam antibiotic solution and preparation method thereof

Abstract

The invention relates to a beta-lactam antibiotic solution, comprising beta-lactam antibiotic and a solvent, wherein the solvent is a mixing solvent formed by 2-pyrrolidone and propylene glycol; and 5-50g of beta-lactam medicine is dissolved in every 100mL of the mixing solvent. The preparation process of the solution is simple, and can adopt a nonaseptic raw material for preparation and a filtering method for degerming. The medicine is evenly dispersed in the solvent in a micromolecule mode which can be absorbed rapidly after entering the organism, can quickly enter the tissue and has high bioavailability, can be used for target animals without being frozen in the environment below 0 DEG C, does not need to oscillate and heat before being used, and can be taken orally, administrated outside intestinal tracts and locally administrated.

Description

technical field [0001] The invention relates to a β-lactam antibiotic pharmaceutical preparation, in particular to a β-lactam antibiotic solution and a preparation method thereof. Background technique [0002] β-lactam antibiotics refer to a large class of antibiotics with a β-lactam ring in their chemical structure, including the most commonly used clinical penicillins and cephalosporins, as well as the newly developed cephamycins, thiamycins, and monocyclic antibiotics. β-lactams and other atypical β-lactam antibiotics. Such antibiotics have the advantages of strong bactericidal activity, low toxicity, wide indications and good clinical curative effect. [0003] The mechanism of action of various β-lactam antibiotics is similar. They can bind to proteins and inhibit cell wall mucopeptide synthase, thereby hindering the synthesis of cell wall mucopeptides, causing bacterial cell wall defects, and bacterial cell swelling and cracking; and can also trigger bacteria autolyso...

AI Technical Summary

Problems solved by technology

[0005] Among them, sterile powders are mostly found in the sodium or potassium salts of penicillin antibiotics and cephalosporin antibiotics. The sterile crystal powder is stable at room temperature and easily soluble in water, but the aqueous solution is unstable at room temperature. Hours, the antibacterial activity declines rapidly, and can produce antigenic degradation products; and before use, it must be diluted with sterile water for injection or sterile saline, and it will be released quickly after injection into the body, and soon reach the peak concentration of the drug in blood, as a treatment Drugs are ideal, but costly

[0006] Suspensions are mostly found in cephalosporin free acid or ester cephalosporins, which are used for subcutaneous or intramuscular injection in animals, but their disadvantages are that the drug effect is slow after being injected into the body, and there is no high blood drug concentration in the initial stage of release, so Simply using suspensions prepared from ester cephalosporins or cephalosporin free acids as therapeutic drugs, the effect is not very satisfactory

[0007] The disadvantages of suspension for injection or sterile powder are: (1) suspension for injection must be prepared using sterile powder, the cost of sterile powder is much higher than the cost of non-sterile powder, and the preparation of sterile powder It needs to invest a lot of time and labor; (2) the suspension cannot be sterilized by filtration, if it is sterilized by filtration, it is easy to remove the active ingredients in the suspension; (3) the drug components and liquid components in the suspension have inhomogeneity (4) The nature of the suspension is unstable, and the drug particles will settle and gather at the bottom of the container after being left for a period of time. Temperature changes and long-term sedimentation of the drug at the bottom of the container will cause compaction and / or recrystallization of the drug; (5) The particle size of the drug in the suspension is directly related to the bioavailability of the drug, and the particle size of the drug can vary. Significantly affect the bioavailability of the drug

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